The present invention relates to novel 1-acyl-2,3-dihydro-4(lH)-quinolinone-4-oxime-O-sulfonic acid compounds, process for producing said compounds, intermediate compounds, novel 1-acyl-2,3-dihydro4(lH)-quinolinone compounds, to produce said compounds and compositions containing said compounds with potent diuretic activity that can be used for treating and/or preventing hypertension, oedema and/or for removing ascites.
For the treatment of hypertension benzothiazide derivatives or so-called loop diuretics have been widely used to lower blood pressure. These agents act mainly on the distal part of renal tubule or the loop of Henle and increase renal excretion of electrolytes and water. Many of these diuretics, however, are known to show several adverse reaction in common, for example, hypokalemia, hyperuricemia, decrease in sugar tolerance and disorder in lipid metabolism.
Diuretic agents have also been used for the treatment of oedema resulting from retention of water and electrolytes based on cardiac or renal insufficiency or on metabolic disorders, but such conventionally used diuretics show only marginal efficacy against retention of ascites which is often observed in the patients with abdominal tumor or liver cirrhosis.
These benzothiazide diuretics and loop diuretics are known to share common chemical substructures.
From the foregoing background, it has been desired to develop novel diuretics that are useful in the treatment of hypertension, oedema and removal of ascites and that do not cause aforementioned adverse reactions by synthesizing compounds whose chemical structures are novel and different from those of known diuretics.